A molecular electronegativity distance vector(M)based on 13 atomic types has been used to describe the structures of 19 conjugates(LHCc)of levofloxacin-thiadiazole HDAC inhibitor(HDACi)and related inhibitory activitie...A molecular electronegativity distance vector(M)based on 13 atomic types has been used to describe the structures of 19 conjugates(LHCc)of levofloxacin-thiadiazole HDAC inhibitor(HDACi)and related inhibitory activities(pH,i=1,2,6)of LHCc against histone deacetylases(HDACs,such as HDAC1,HDAC2 and HDAC6).The quantitative structure-activity relationships(QSAR)were established by using leaps-and-bounds regression analysis for the inhibitory activities(pH)of 19 above compounds to HDAC1,HDAC2 and HDAC6 along with M.The correlation coefficients(R~2)and the leave-one-out(LOO)cross validation Rfor the pH,pHand pHmodels were 0.976 and 0.949;0.985 and 0.977;0.976 and 0.932,respectively.The QSAR models had favorable correlations,as well as robustness and good prediction capability by R~2,F,R~2,A,Fand Vtests.Validated by using 3876 training sets,the models have good external prediction ability.The results indicate that the molecular structural units:–CH–(g=1,2),–NH,–OH,=O,–O–and–S–are the main factors which can affect the inhibitory activity of pH,pHas well as pHbioactivities of these compounds directly.Accordingly,the main interactions between HDACs inhibitor and HDACs are hydrophobic interaction,hydrogen bond,and coordination with Znto form compounds,which is consistent with the results in reports.展开更多
Objective:To explore pancreatic lipase inhibitory activity under different extraction conditions in order to track the most potent extract.Methods:The methanolic extract and its fractions in solvents of increasing pol...Objective:To explore pancreatic lipase inhibitory activity under different extraction conditions in order to track the most potent extract.Methods:The methanolic extract and its fractions in solvents of increasing polarity,ether,chloroform,ethyl acetate,n-butanol and water,were made through cold maceration.Extracts in ethanol,ethyl acetate,acetone and chloroform were similarly prepared.Aqueous extract was prepared through hot decoction method.A reported method was used to determine lipase inhibitory activity of extracts and fractions over wide ranges of concentrations.Results:The extracts and fractions exhibited concentration dependent activity.The IC50(μg/mL)values of methanolic,ethanolic,chloroform,ethyl acetate,acetone,ethyl acetate(after washing with water)and aqueous decoction were 293.40,266.47,157.59,182.12,352.34,257.00,and 190.00,respectively.The activity of chloroform,ethyl acetate and aqueous extracts were close to that of the drug orlistat(IC50 146μg/mL).Out of the fractions of the methanolic extract,the chloroform fraction was most active(IC50 189.6μg/mL).The order of inhibitory activity of the fractions was as follows:chloroform>ether>n-butanolic>aqueous>ethyl acetate.The GC/MS analysis of the most active chloroform faction showed the presence of hexadecanoic acid,methyl hexadecanoate,isopropyl palmitate,methyl 9,12-octadecadienate,and methyl 9,12,15-octadecatrienoate.Conclusions:The study suggests that Lagenaria siceraria has potential to inhibit pancreatic lipase activity,suppressing lipid digestion and thereby diminishing entry of lipids into the body.Regular intake of aqueous decoction of the fruit may therefore be recommended for control of obesity.Fatty acids and their esters may play role as inhibitors of lipase.展开更多
[Objective] This study aimed to analyze the in vitro inhibitory activity of Shisandra chinensis and Polygonatum sibiricum against Vibrio harveyi and its biofilms. [Result] By agar diffusion test, in vit...[Objective] This study aimed to analyze the in vitro inhibitory activity of Shisandra chinensis and Polygonatum sibiricum against Vibrio harveyi and its biofilms. [Result] By agar diffusion test, in vitro inhibitory activity of 5. chinensis and P. sibiricum against V. harveyi was investigated. The minimal inhibitory concentration （ MIC） and minimal bactericidal concentration （MBC） of 5. chinensis and P. sibiricum against V. harveyi were determined by doubling dilution meth-od. The inhibitory activity of 5. chinensis and P. sibiricum on the formation of V. harveyi biofilms was evaluated by modified MTT assay. [ Result ] Both 5. chinen-sis and P. sibiricum had inhibitory activity against V. harveyi. The inhibition zone diameter of 5. chinensis against V. harveyi was 17. 95 mm; MIC and MBC of 5. chinensis were both 3.125 mg/ml. The inhibition zone diameter of P. sibiricum against V. harveyi was 12. 22 mm; MIC and MBC of P. sibiricum were 3.125 and 6.250 mg/ml, respectively. When the concentration was higher than 6. 25 mg/ml, 5. chinensis decoction had extremely significant inhibitory activity against V. harveyi （P 〈 0. 01） ; when the concentration was higher than 3. 125 mg/ml, P. sibiricum had extremely significant inhibitory activity against V. harveyi （P 〈0. 01）. [ Conclusion] 5. chinensis and P. sibiricum could significantly inhibit V. harveyi and its biofilms.展开更多
The objective of this study was to isolate and identify the intracellular bioactive peptides from mouse lymphocytes before and after lipopolysaccharide(LPS)stimulation,to explore novel peptides and to research the bio...The objective of this study was to isolate and identify the intracellular bioactive peptides from mouse lymphocytes before and after lipopolysaccharide(LPS)stimulation,to explore novel peptides and to research the bioactive function.Mouse spleen lymphocytes were isolated and cultured with LPS stimulation(experimental group)or not(control group)to collect intracellular peptides.Totally 385 peptides were analyzed by nanoliter liquid phase-Q Exactive quadrupole ultra-high resolution orbitrap mass spectrometer(Nano LC-Q Exactive Plus)and identifi ed by PEAKS X software.After compared with peptides reported,131 novel peptides were discovered,which then were predicted bioactivity by Peptide Ranker and 6 peptides with high bioactivity were predicted function by BIOPEP-UMW database.Prediction data showed that they may have dipeptidyl peptidase IV(DPP-IV)inhibitory activity.Finally,two peptides showed better potent inhibition were verifi ed with competitive and noncompetitive modes.展开更多
The replacement of the disulfide bridge of CPI-1, a peptide inhibitor of light chain of Botulinum toxin serotype A, with the thioether-containing and biscarba-containing diaminodiacid bridge leads to a significant dec...The replacement of the disulfide bridge of CPI-1, a peptide inhibitor of light chain of Botulinum toxin serotype A, with the thioether-containing and biscarba-containing diaminodiacid bridge leads to a significant decrease in the degradation by trypsin and increase in the detoxification activity in vivo, the addition of hydrophobic or positive amino acid at C-terminus of modified peptides further improves the inhibitory activity.展开更多
The purpose of this study was to develop liposomal formulations of Asparagus racemosus root extract(AR1-6)as well as evaluate the physicochemical properties and in vitro tyrosinase inhibitory activity.Liposomes compos...The purpose of this study was to develop liposomal formulations of Asparagus racemosus root extract(AR1-6)as well as evaluate the physicochemical properties and in vitro tyrosinase inhibitory activity.Liposomes composed of AR1-6 to lipid weight ratio of 1:10 and lecithin(LEC)or Phospholipon90G(PC90G)as structural phospholipid at 7:3 molar ratio to CHOL were prepared by various methods,i.e.chloroform-film(CF),reverse-phase evaporation(REV),polyol dilution(PD),and freeze-drying of monophase solution(MFD)methods.The results revealed that vesicles prepared by CF and MFD were multilamellar whereas those prepared by REV and PD were oligolamellar in nature with particle sizes ranging from 0.26 to 13.83 mm.The zeta potentials were in the range of1.5 to39.3 mV.AR1-6 liposomes with LEC possessed significantly higher entrapment than those with PC90G.The highest entrapment efficiency and in vitro tyrosinase inhibitory activity of 69.08%and 25%,respectively,were obtained from liposomes having LEC and prepared by PD method.The tyrosinase inhibitory activity were in the rank order of LEC>PC90G,and PD>CF>REV>MFD.It could be concluded that the mechanism of vesicle forming in each method of preparation was the key factor influencing physicochemical properties,particularly vesicle type,size,surface charge,and entrapment,which were well correlated with the biological activity.展开更多
A chloro-bridged dinuclear copper（H） complex with ligand 2-pyridylme-thylene- furfurylamine has been synthesized and characterized by single-crystal X-ray diffraction, and its inhibitory activity on xanthine oxidase...A chloro-bridged dinuclear copper（H） complex with ligand 2-pyridylme-thylene- furfurylamine has been synthesized and characterized by single-crystal X-ray diffraction, and its inhibitory activity on xanthine oxidase （XO） was also evaluated. It crystallizes in the triclinic system, space group P 1 with a = 8.0441（16）, b = 8.5663（17）, c = 10.060（2）A, α = 77.52（3）, β = 72.04（3）, γ = 70.12（3）°, V = 615.3（2）A^3, Z = 1, Dc = 1.731 g/cm^3, F（000） = 322, the final R = 0.0401 and wR = 0.0934 for 1971 observed reflections with I 〉 2σ（I）. X-ray analysis reveals that the Cu（II） cation is five-coordinated by two N atoms of Schiff base and three Cl anions. The C-H…Cl intermolecular and intramolecular hydrogen bonds connect the molecules to form a three-dimensional network. This copper（II） complex shows more potent inhibitory activity against XO with IC50 = 3.48μM than the standard inhibitor allopurinol.展开更多
Eight 16,17-pyrazo-annulated steroidal derivatives were synthesized and evaluated in vitro vascular endothelial growth factor （VEGF） inhibitory activity with 2-methoxyestradiol （2-ME） as the reference compound. Mo...Eight 16,17-pyrazo-annulated steroidal derivatives were synthesized and evaluated in vitro vascular endothelial growth factor （VEGF） inhibitory activity with 2-methoxyestradiol （2-ME） as the reference compound. Most of the compounds showed potent VEGF inhibitory activity with ECs0 values of micromolar or submicromolar range. Among them, the compounds 3 and 8 exhibited similar EC50 values and obviously better TI values compared with 2-ME.展开更多
Suaeda physophora Pall.is a kind of desert plant mostly growing in saline habitats in Xinjiang Uygur Autonomous Region.In order to have a better utilization of halophytes,a screening for ACE inhibitors from halophytes...Suaeda physophora Pall.is a kind of desert plant mostly growing in saline habitats in Xinjiang Uygur Autonomous Region.In order to have a better utilization of halophytes,a screening for ACE inhibitors from halophytes growing in Xinjiang was carried out.The result showed that the 70%EtOH extract and n-BuOH extract of S.physophora Pall.possessed significant ACE inhibitory activities.So we focused on its biochemical constituents firstly.One new quinazoline alkaloid,namely Suaedine(1),along with six known compounds(2–7)was isolated from the aerial parts of S.physophora Pall.The structure of the new quinazoline alkaloid was established by one-and two-dimensional nuclear magnetic resonance,optical rotation and mass spectrometry analysis.The flavonoid compounds(2–4)and phenolic compound(5)exhibited significant ACE activities.It was the first time to focus on the chemical constituents and bioactivities of this plant.展开更多
Acarbose is a potent glycosidase inhibitor widely used in the clinical treatment of type 2 diabetes mellitus(T2DM).Various acarbose analogs have been identified while exploring compounds with improved pharmacological ...Acarbose is a potent glycosidase inhibitor widely used in the clinical treatment of type 2 diabetes mellitus(T2DM).Various acarbose analogs have been identified while exploring compounds with improved pharmacological properties.In this study,we found that AcbE from Actinoplanes sp.SE50/110 catalyzes the production of acarbose analogs that exhibit significantly improved inhibitory activity towardsα-amylase than acarbose.Recombinant AcbE mainly catalyzed the formation of two new compounds,namely acarstatins A and B,using acarbose as substrate.Using high-resolution mass spectrometry,nuclear magnetic resonance,and glycosidase hydrolysis,we elucidated their chemical structures as O-α-d-maltosyl-(1→4)-acarbose and O-α-d-maltotriosyl-(1→4)-acarbose,respectively.Acarstatins A and B exhibited 1584-and 1478-fold greater inhibitory activity towards human salivaryα-amylase than acarbose.Furthermore,both acarstatins A and B exhibited complete resistance to microbiome-derived acarbose kinase 1-mediated phosphorylation and partial resistance to acarbose-preferred glucosidase-mediated hydrolysis.Therefore,acarstatins A and B have great potential as candidate therapeutic agents for T2DM.展开更多
A simple and efficient HPLC method was developed for quality analysis of flavonoids from Impatiens balsamina L.(IBL)flowers,which were collected from Xingjiang,Anhui,Henan,and Hubei provinces in China.The flavonoids s...A simple and efficient HPLC method was developed for quality analysis of flavonoids from Impatiens balsamina L.(IBL)flowers,which were collected from Xingjiang,Anhui,Henan,and Hubei provinces in China.The flavonoids substances in IBL were determined by HPLC through methyl alcohol ultrasonic extraction.A mixture of展开更多
Tumor necrosis factor α （TNF-α） and interferon-γ （IFN-γ） are cytokines with strong antitumor activities. They were reacted with a photoactive arylazide-4-azidobenzoic acid, resulting in photoactive TNF-α and ...Tumor necrosis factor α （TNF-α） and interferon-γ （IFN-γ） are cytokines with strong antitumor activities. They were reacted with a photoactive arylazide-4-azidobenzoic acid, resulting in photoactive TNF-α and IFN-γ. The infrared （IR） spectra of these products showed the characteristic absorption of an azido group at 2127 cm^-1. By photo-immobilization, this modified TNF-α and IFN-γ were immobilized on polystyrene membranes for cell culture to prepare biomaterials. The micro-morphology of photoactive cytokines was observed with a scanning electron microscope （SEM）. The inhibitory effect on growth of Hela cells and inducing apoptosis activity of these two cytokines were analyzed by growth curve, transmission electron microscope （TEM） and fluorescence active cell sorter （FACS）. The results showed that co-immobilization of IFN-γ and TNF-α had significant inhibitory effect on growth of Hela cells, inhibitory rate up to 82%, and IFN-γ had obviously synergistic action.展开更多
Acorus tatarinowii Schott is a traditional Chinese medicine plant and has multiple bioactivities in medicine and pesticide field.In this study,the antifungal compound 1,2-dimethoxy-4(2-propenyl)benzene was isolated fr...Acorus tatarinowii Schott is a traditional Chinese medicine plant and has multiple bioactivities in medicine and pesticide field.In this study,the antifungal compound 1,2-dimethoxy-4(2-propenyl)benzene was isolated from A.tatarinowii Schott by activity-directed isolation method,and the inhibitory activity of the extract and 1,2-dimethoxy-4(2-propenyl)benzene against seven plant pathogenic fungi was evaluated.The results showed that the extract and 1,2-dimethoxy-4(2-propenyl)benzene had high inhibitory activity against hyphal growth of Thielaviopsis paradoxa(de Seynes)V.Hohnel,Pestalotia mangiferae P.Henn.,Fusarium oxysporum f.sp.niveum(E.F.Smith)Syn.et Hans.,Alternaria alternate Tanaka,Colletotrichum musae(Berk et Curt)V.Arx,Sphaceloma fawcettii Jenk.,and Mycosphaerella sentina(Fr.)Schroter.The EC50 values of extract were 1.6162,1.6811,1.1253,3.5771,1.7024,2.2284,and 2.2221 g L^-1,respectively,and the EC50 values of 1,2-dimethoxy-4(2-propenyl)benzene were 0.1021,0.0997,0.0805,0.1742,0.1503,0.1853,and 0.1924 g L^-1,respectively.1,2-Dimethoxy-4(2-propenyl)benzene also inhibited spores germination of T.paradoxa(de Seynes)V.Hohnel and F.oxysporum f.sp.niveum(E.F.Smith)Syn.et Hans.,with the inhibitory rates of 98.81 and 100%at a concentration of 0.4 g L^-1 after 8 h,respectively.1,2-Dimethoxy-4(2-propenyl)benzene is a potential botanical antifungal agent for controling of plant fungal diseases.展开更多
Background:To explore the differences of 14 batches of Citri Reticulatae Pericarpium from different regions.Methods:The main aim of this study was to develop a high-performance liquid chromatography method-photodiode ...Background:To explore the differences of 14 batches of Citri Reticulatae Pericarpium from different regions.Methods:The main aim of this study was to develop a high-performance liquid chromatography method-photodiode array detection for determining the contents of five flavonoids and the chromatographic fingerprints of Citri Reticulatae Pericarpium from different regions.Theα-glucosidase inhibitory activities and antioxidant properties of Citri Reticulatae Pericarpium,based on free-radical scavenging assays against 1,1-diphenyl-2-picrylhydrazyl,2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid),and hydroxyl radicals,were estimated and compared.Results:Among the tested compounds,the content of hesperidin(13.386-68.235 mg/g)was the highest and that of hesperitin(0.045-0.277 mg/g)was the lowest.In comparing different sources of Citri Reticulatae Pericarpium,the contents of narirutin in Citri Reticulatae Pericarpium from Guangdong(0.824-0.851 mg/g)and Sichuan(1.069-1.204 mg/g)provinces of China were lower than in other provinces.In contrast,nobiletin(8.429-12.237 mg/g)and tangeretin(3.947-4.613 mg/g)were most abundant in Guangdong sources of Citri Reticulatae Pericarpium,followed by samples from Sichuan Province(nobiletin:6.761-7.658 mg/g;tangeretin:3.422-3.933 mg/g).Correlation analysis showed that nobiletin and tangeretin were the main contributors to the antioxidant capacity,and narirutin was the main active component inhibiting theα-glucosidase activity of Citri Reticulatae Pericarpium.Conclusion:This work revealed that the intrinsic quality of Citri Reticulatae Pericarpium was affected by different growing regions,which provides a scientific basis for controlling the quality of Citri Reticulatae Pericarpium and rationally developing and utilizing Citri Reticulatae Pericarpium.展开更多
One new spirocyclic alkaloid,5-isopentenyl-cryptoechinuline D(1),along with 11 known compounds(2–12),were iso-lated from a marine fungus Aspergillus ruber TX-M4-1.The structures of compounds 1–12 were elucidated by ...One new spirocyclic alkaloid,5-isopentenyl-cryptoechinuline D(1),along with 11 known compounds(2–12),were iso-lated from a marine fungus Aspergillus ruber TX-M4-1.The structures of compounds 1–12 were elucidated by spectroscopic evi-dences.Compound 1 was initially isolated as an enantiomer,and further separation of 1 by chiral HPLC afforded a pair of enantio-mers,including(-)-5-isopentenyl-cryptoechinuline D(1a)and(+)-5-isopentenyl-cryptoechinuline D(1b).Their absolute configura-tions were elucidated by ECD spectroscopic data.Compounds 1a,5 and 10 could inhibit thioredoxin reductase(TrxR)activity with IC50 values of 6.2,36.3 and 18.6μmol L^(-1),respectively.Surface plasmon resonance(SPR)study also demonsrated the interactions between compounds 6,8 and Niemann-Pick C1 Like 1(NPC1L1)respectively,which indicate that compounds 6 and 8 are potential NPC1L1 inhibitors.展开更多
Listeria monocytogenes(LM),a Gram-positive facultative intracellular bacterium,can be used as an effective exogenous antigen expression vector in tumor-target therapy.But for successful clinical application,it is nece...Listeria monocytogenes(LM),a Gram-positive facultative intracellular bacterium,can be used as an effective exogenous antigen expression vector in tumor-target therapy.But for successful clinical application,it is necessary to construct attenuated LM stain that is safe yet retains the potency of LM based on the full virulent pathogen.In this study,attenuated LM and recombinants of LM expressing melanoma inhibitory activity(MIA) were constructed successfully.The median lethal dose(LD 50) and invasion efficiency of attenuated LM strains were detected.The recombinants were utilized for immunotherapy of animal model of B16F10 melanoma.The level of MIA mRNA expression in tumor tissue was detected by using real-time polymerase chain reaction(PCR) with specific sequence,meanwhile the anti-tumor immune response was assayed by flow cytometric analysis and enzyme-linked immunosorbent spot(ELISPOT) assay.The results showed the toxicity and invasiveness of attenuated LM were decreased as compared with LM,and attenuated LM expressing MIA,especially the double-genes attenuated LM recombinant,could significantly induce anti-tumor immune response and inhibit tumor growth.This study implicates attenuated LM may be a safer and more effective vector for immunotherapy of melanoma.展开更多
Steroid saponins are secondary metabolites with multiple medicinal values that are found in large quantities in natural medicines,especially Vernonia amygdalina,a famous nature medicine for the treatment of tonsilliti...Steroid saponins are secondary metabolites with multiple medicinal values that are found in large quantities in natural medicines,especially Vernonia amygdalina,a famous nature medicine for the treatment of tonsillitis,diabetes,pneumonia.The current study was designed to combine molecular networking(MN)with diagnostic ions for rapid identification ofΔ^(7,9(11))stigmastane-type saponins which were theα-glucosidase inhibitory active substances in V.amygdalina.First,theα-glucosidase inhibitory activities of fiveΔ^(7,9(11))stigmastane-type steroid saponins that were previously isolated were screened,which indicated that theΔ^(7,9(11))stigmastane-type steroid saponin was one of the active constituents responsible for ameliorating diabetes.Furthermore,a strategy was proposed to identify stigmastane-type steroid saponins and verify the plausibility of derived fragmentation pathways by applying MN,MolNetEnhancer and unsupervised substructure annotation(MS2LDA).Based on this strategy,other sevenΔ^(7,9(11))stigmastane-type steroid saponins were identified from this plant.Our research provide scientific evidence for the antidiabetic potential of the steroid saponin-rich extract of V.amygdalina leaf.展开更多
Ten cucurbitane-type triterpene glycosides,including five new compounds named charantosides H(1),J(2),K(3),momor-characoside A(4),goyaglycoside-l(5),and five known compounds(6-10),were isolated from the EtOAc extract ...Ten cucurbitane-type triterpene glycosides,including five new compounds named charantosides H(1),J(2),K(3),momor-characoside A(4),goyaglycoside-l(5),and five known compounds(6-10),were isolated from the EtOAc extract of Momor-dica charantia fruits.The chemical structures of these compounds were identified by 1D and 2D NMR and HRESIMS spectroscopic analyses.Configurations of new compounds were determined by ROESY correlations and comparison of their 13C NMR data with literature reported values.All compounds were evaluated for their inhibition againstα-glucosidase,in which compounds 2,5,7,8,9 showed moderate inhibitory activities with IC50 values ranging from 28.40 to 63.26μM comparing with the positive control(acarbose,IC5087.65±6.51μM).展开更多
基金supported by the National Natural Science Foundation of China(21473081,21075138)special fund of State Key Laboratory of Structure Chemistry(20160028)
文摘A molecular electronegativity distance vector(M)based on 13 atomic types has been used to describe the structures of 19 conjugates(LHCc)of levofloxacin-thiadiazole HDAC inhibitor(HDACi)and related inhibitory activities(pH,i=1,2,6)of LHCc against histone deacetylases(HDACs,such as HDAC1,HDAC2 and HDAC6).The quantitative structure-activity relationships(QSAR)were established by using leaps-and-bounds regression analysis for the inhibitory activities(pH)of 19 above compounds to HDAC1,HDAC2 and HDAC6 along with M.The correlation coefficients(R~2)and the leave-one-out(LOO)cross validation Rfor the pH,pHand pHmodels were 0.976 and 0.949;0.985 and 0.977;0.976 and 0.932,respectively.The QSAR models had favorable correlations,as well as robustness and good prediction capability by R~2,F,R~2,A,Fand Vtests.Validated by using 3876 training sets,the models have good external prediction ability.The results indicate that the molecular structural units:–CH–(g=1,2),–NH,–OH,=O,–O–and–S–are the main factors which can affect the inhibitory activity of pH,pHas well as pHbioactivities of these compounds directly.Accordingly,the main interactions between HDACs inhibitor and HDACs are hydrophobic interaction,hydrogen bond,and coordination with Znto form compounds,which is consistent with the results in reports.
基金Pakistan Science Foundation(PSF),Islamabad,for its financial support for the study(PSF/NSLP/P-FCCU)
文摘Objective:To explore pancreatic lipase inhibitory activity under different extraction conditions in order to track the most potent extract.Methods:The methanolic extract and its fractions in solvents of increasing polarity,ether,chloroform,ethyl acetate,n-butanol and water,were made through cold maceration.Extracts in ethanol,ethyl acetate,acetone and chloroform were similarly prepared.Aqueous extract was prepared through hot decoction method.A reported method was used to determine lipase inhibitory activity of extracts and fractions over wide ranges of concentrations.Results:The extracts and fractions exhibited concentration dependent activity.The IC50(μg/mL)values of methanolic,ethanolic,chloroform,ethyl acetate,acetone,ethyl acetate(after washing with water)and aqueous decoction were 293.40,266.47,157.59,182.12,352.34,257.00,and 190.00,respectively.The activity of chloroform,ethyl acetate and aqueous extracts were close to that of the drug orlistat(IC50 146μg/mL).Out of the fractions of the methanolic extract,the chloroform fraction was most active(IC50 189.6μg/mL).The order of inhibitory activity of the fractions was as follows:chloroform>ether>n-butanolic>aqueous>ethyl acetate.The GC/MS analysis of the most active chloroform faction showed the presence of hexadecanoic acid,methyl hexadecanoate,isopropyl palmitate,methyl 9,12-octadecadienate,and methyl 9,12,15-octadecatrienoate.Conclusions:The study suggests that Lagenaria siceraria has potential to inhibit pancreatic lipase activity,suppressing lipid digestion and thereby diminishing entry of lipids into the body.Regular intake of aqueous decoction of the fruit may therefore be recommended for control of obesity.Fatty acids and their esters may play role as inhibitors of lipase.
基金Supported by Project of Enhancing School with Innovation of Guangdong Ocean University(GDOU2015050216)Major Program for the Fundamental Research of the Department of Education of Guangdong Province(2014GKXM046)International Cooperation Innovation Platform Project of Universities in Guangdong Province(2013gjhz0008)
文摘[Objective] This study aimed to analyze the in vitro inhibitory activity of Shisandra chinensis and Polygonatum sibiricum against Vibrio harveyi and its biofilms. [Result] By agar diffusion test, in vitro inhibitory activity of 5. chinensis and P. sibiricum against V. harveyi was investigated. The minimal inhibitory concentration （ MIC） and minimal bactericidal concentration （MBC） of 5. chinensis and P. sibiricum against V. harveyi were determined by doubling dilution meth-od. The inhibitory activity of 5. chinensis and P. sibiricum on the formation of V. harveyi biofilms was evaluated by modified MTT assay. [ Result ] Both 5. chinen-sis and P. sibiricum had inhibitory activity against V. harveyi. The inhibition zone diameter of 5. chinensis against V. harveyi was 17. 95 mm; MIC and MBC of 5. chinensis were both 3.125 mg/ml. The inhibition zone diameter of P. sibiricum against V. harveyi was 12. 22 mm; MIC and MBC of P. sibiricum were 3.125 and 6.250 mg/ml, respectively. When the concentration was higher than 6. 25 mg/ml, 5. chinensis decoction had extremely significant inhibitory activity against V. harveyi （P 〈 0. 01） ; when the concentration was higher than 3. 125 mg/ml, P. sibiricum had extremely significant inhibitory activity against V. harveyi （P 〈0. 01）. [ Conclusion] 5. chinensis and P. sibiricum could significantly inhibit V. harveyi and its biofilms.
文摘The objective of this study was to isolate and identify the intracellular bioactive peptides from mouse lymphocytes before and after lipopolysaccharide(LPS)stimulation,to explore novel peptides and to research the bioactive function.Mouse spleen lymphocytes were isolated and cultured with LPS stimulation(experimental group)or not(control group)to collect intracellular peptides.Totally 385 peptides were analyzed by nanoliter liquid phase-Q Exactive quadrupole ultra-high resolution orbitrap mass spectrometer(Nano LC-Q Exactive Plus)and identifi ed by PEAKS X software.After compared with peptides reported,131 novel peptides were discovered,which then were predicted bioactivity by Peptide Ranker and 6 peptides with high bioactivity were predicted function by BIOPEP-UMW database.Prediction data showed that they may have dipeptidyl peptidase IV(DPP-IV)inhibitory activity.Finally,two peptides showed better potent inhibition were verifi ed with competitive and noncompetitive modes.
基金supported by the National Key Research and Development Project of China (2017YFC1200905)。
文摘The replacement of the disulfide bridge of CPI-1, a peptide inhibitor of light chain of Botulinum toxin serotype A, with the thioether-containing and biscarba-containing diaminodiacid bridge leads to a significant decrease in the degradation by trypsin and increase in the detoxification activity in vivo, the addition of hydrophobic or positive amino acid at C-terminus of modified peptides further improves the inhibitory activity.
基金The financial support from the Thai Herbal NanoCosmeceuticals Coordinated Research Program,National Nanotechnology Center,National Science and Technology Development Agency,Thailand is gratefully acknowledged.
文摘The purpose of this study was to develop liposomal formulations of Asparagus racemosus root extract(AR1-6)as well as evaluate the physicochemical properties and in vitro tyrosinase inhibitory activity.Liposomes composed of AR1-6 to lipid weight ratio of 1:10 and lecithin(LEC)or Phospholipon90G(PC90G)as structural phospholipid at 7:3 molar ratio to CHOL were prepared by various methods,i.e.chloroform-film(CF),reverse-phase evaporation(REV),polyol dilution(PD),and freeze-drying of monophase solution(MFD)methods.The results revealed that vesicles prepared by CF and MFD were multilamellar whereas those prepared by REV and PD were oligolamellar in nature with particle sizes ranging from 0.26 to 13.83 mm.The zeta potentials were in the range of1.5 to39.3 mV.AR1-6 liposomes with LEC possessed significantly higher entrapment than those with PC90G.The highest entrapment efficiency and in vitro tyrosinase inhibitory activity of 69.08%and 25%,respectively,were obtained from liposomes having LEC and prepared by PD method.The tyrosinase inhibitory activity were in the rank order of LEC>PC90G,and PD>CF>REV>MFD.It could be concluded that the mechanism of vesicle forming in each method of preparation was the key factor influencing physicochemical properties,particularly vesicle type,size,surface charge,and entrapment,which were well correlated with the biological activity.
基金the National Natural Science Foundation of China (No. 649620)
文摘A chloro-bridged dinuclear copper（H） complex with ligand 2-pyridylme-thylene- furfurylamine has been synthesized and characterized by single-crystal X-ray diffraction, and its inhibitory activity on xanthine oxidase （XO） was also evaluated. It crystallizes in the triclinic system, space group P 1 with a = 8.0441（16）, b = 8.5663（17）, c = 10.060（2）A, α = 77.52（3）, β = 72.04（3）, γ = 70.12（3）°, V = 615.3（2）A^3, Z = 1, Dc = 1.731 g/cm^3, F（000） = 322, the final R = 0.0401 and wR = 0.0934 for 1971 observed reflections with I 〉 2σ（I）. X-ray analysis reveals that the Cu（II） cation is five-coordinated by two N atoms of Schiff base and three Cl anions. The C-H…Cl intermolecular and intramolecular hydrogen bonds connect the molecules to form a three-dimensional network. This copper（II） complex shows more potent inhibitory activity against XO with IC50 = 3.48μM than the standard inhibitor allopurinol.
基金supported by grants from the National Natural Science Foundation of China awarded to P.Xia (No.20272010) and Y.Chen(No.30200348 and 30873164)the National Drug Innovative Program(No.2009ZX09301-011) for partial support
文摘Eight 16,17-pyrazo-annulated steroidal derivatives were synthesized and evaluated in vitro vascular endothelial growth factor （VEGF） inhibitory activity with 2-methoxyestradiol （2-ME） as the reference compound. Most of the compounds showed potent VEGF inhibitory activity with ECs0 values of micromolar or submicromolar range. Among them, the compounds 3 and 8 exhibited similar EC50 values and obviously better TI values compared with 2-ME.
基金supported by the National Natural Science Foundation of China(81001371)the Science and Technology Foundation of Dalian city(2011J21DW012).
文摘Suaeda physophora Pall.is a kind of desert plant mostly growing in saline habitats in Xinjiang Uygur Autonomous Region.In order to have a better utilization of halophytes,a screening for ACE inhibitors from halophytes growing in Xinjiang was carried out.The result showed that the 70%EtOH extract and n-BuOH extract of S.physophora Pall.possessed significant ACE inhibitory activities.So we focused on its biochemical constituents firstly.One new quinazoline alkaloid,namely Suaedine(1),along with six known compounds(2–7)was isolated from the aerial parts of S.physophora Pall.The structure of the new quinazoline alkaloid was established by one-and two-dimensional nuclear magnetic resonance,optical rotation and mass spectrometry analysis.The flavonoid compounds(2–4)and phenolic compound(5)exhibited significant ACE activities.It was the first time to focus on the chemical constituents and bioactivities of this plant.
基金This work was supported by the National Key Research and Development Program of China(grant No.2021YFC2100600)National Natural Science Foundation of China(grant No.31830104)Science and Technology Commission of Shanghai Municipality(grant Nos.19JC1413000 and 19430750600)to L.B.We thank the Core Facility and Technical Service Center for SLSB and the Instrumental Analysis Center in SJTU for data collection.
文摘Acarbose is a potent glycosidase inhibitor widely used in the clinical treatment of type 2 diabetes mellitus(T2DM).Various acarbose analogs have been identified while exploring compounds with improved pharmacological properties.In this study,we found that AcbE from Actinoplanes sp.SE50/110 catalyzes the production of acarbose analogs that exhibit significantly improved inhibitory activity towardsα-amylase than acarbose.Recombinant AcbE mainly catalyzed the formation of two new compounds,namely acarstatins A and B,using acarbose as substrate.Using high-resolution mass spectrometry,nuclear magnetic resonance,and glycosidase hydrolysis,we elucidated their chemical structures as O-α-d-maltosyl-(1→4)-acarbose and O-α-d-maltotriosyl-(1→4)-acarbose,respectively.Acarstatins A and B exhibited 1584-and 1478-fold greater inhibitory activity towards human salivaryα-amylase than acarbose.Furthermore,both acarstatins A and B exhibited complete resistance to microbiome-derived acarbose kinase 1-mediated phosphorylation and partial resistance to acarbose-preferred glucosidase-mediated hydrolysis.Therefore,acarstatins A and B have great potential as candidate therapeutic agents for T2DM.
文摘A simple and efficient HPLC method was developed for quality analysis of flavonoids from Impatiens balsamina L.(IBL)flowers,which were collected from Xingjiang,Anhui,Henan,and Hubei provinces in China.The flavonoids substances in IBL were determined by HPLC through methyl alcohol ultrasonic extraction.A mixture of
基金This work was supported by the China Postdoctoral Science Foundation under grant No.2004035588.
文摘Tumor necrosis factor α （TNF-α） and interferon-γ （IFN-γ） are cytokines with strong antitumor activities. They were reacted with a photoactive arylazide-4-azidobenzoic acid, resulting in photoactive TNF-α and IFN-γ. The infrared （IR） spectra of these products showed the characteristic absorption of an azido group at 2127 cm^-1. By photo-immobilization, this modified TNF-α and IFN-γ were immobilized on polystyrene membranes for cell culture to prepare biomaterials. The micro-morphology of photoactive cytokines was observed with a scanning electron microscope （SEM）. The inhibitory effect on growth of Hela cells and inducing apoptosis activity of these two cytokines were analyzed by growth curve, transmission electron microscope （TEM） and fluorescence active cell sorter （FACS）. The results showed that co-immobilization of IFN-γ and TNF-α had significant inhibitory effect on growth of Hela cells, inhibitory rate up to 82%, and IFN-γ had obviously synergistic action.
基金supported by the Key Laboratory for the Chemistry and Molecular Engineering of Medicinal Resources(Guangxi Normal University,China),Ministry of Education of China(07109001-11)Guangxi Natural Science Fund Project,China(0991097)
文摘Acorus tatarinowii Schott is a traditional Chinese medicine plant and has multiple bioactivities in medicine and pesticide field.In this study,the antifungal compound 1,2-dimethoxy-4(2-propenyl)benzene was isolated from A.tatarinowii Schott by activity-directed isolation method,and the inhibitory activity of the extract and 1,2-dimethoxy-4(2-propenyl)benzene against seven plant pathogenic fungi was evaluated.The results showed that the extract and 1,2-dimethoxy-4(2-propenyl)benzene had high inhibitory activity against hyphal growth of Thielaviopsis paradoxa(de Seynes)V.Hohnel,Pestalotia mangiferae P.Henn.,Fusarium oxysporum f.sp.niveum(E.F.Smith)Syn.et Hans.,Alternaria alternate Tanaka,Colletotrichum musae(Berk et Curt)V.Arx,Sphaceloma fawcettii Jenk.,and Mycosphaerella sentina(Fr.)Schroter.The EC50 values of extract were 1.6162,1.6811,1.1253,3.5771,1.7024,2.2284,and 2.2221 g L^-1,respectively,and the EC50 values of 1,2-dimethoxy-4(2-propenyl)benzene were 0.1021,0.0997,0.0805,0.1742,0.1503,0.1853,and 0.1924 g L^-1,respectively.1,2-Dimethoxy-4(2-propenyl)benzene also inhibited spores germination of T.paradoxa(de Seynes)V.Hohnel and F.oxysporum f.sp.niveum(E.F.Smith)Syn.et Hans.,with the inhibitory rates of 98.81 and 100%at a concentration of 0.4 g L^-1 after 8 h,respectively.1,2-Dimethoxy-4(2-propenyl)benzene is a potential botanical antifungal agent for controling of plant fungal diseases.
基金supported by the National Natural Science Foundation of China(No.81872956)National Key R&D Program of China(No.2019YFC1710604)+1 种基金Key Project at Central Government Level(No.2060302)the Science and Technology Project of Tianjin(No.18ZXXYSY00080).
文摘Background:To explore the differences of 14 batches of Citri Reticulatae Pericarpium from different regions.Methods:The main aim of this study was to develop a high-performance liquid chromatography method-photodiode array detection for determining the contents of five flavonoids and the chromatographic fingerprints of Citri Reticulatae Pericarpium from different regions.Theα-glucosidase inhibitory activities and antioxidant properties of Citri Reticulatae Pericarpium,based on free-radical scavenging assays against 1,1-diphenyl-2-picrylhydrazyl,2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid),and hydroxyl radicals,were estimated and compared.Results:Among the tested compounds,the content of hesperidin(13.386-68.235 mg/g)was the highest and that of hesperitin(0.045-0.277 mg/g)was the lowest.In comparing different sources of Citri Reticulatae Pericarpium,the contents of narirutin in Citri Reticulatae Pericarpium from Guangdong(0.824-0.851 mg/g)and Sichuan(1.069-1.204 mg/g)provinces of China were lower than in other provinces.In contrast,nobiletin(8.429-12.237 mg/g)and tangeretin(3.947-4.613 mg/g)were most abundant in Guangdong sources of Citri Reticulatae Pericarpium,followed by samples from Sichuan Province(nobiletin:6.761-7.658 mg/g;tangeretin:3.422-3.933 mg/g).Correlation analysis showed that nobiletin and tangeretin were the main contributors to the antioxidant capacity,and narirutin was the main active component inhibiting theα-glucosidase activity of Citri Reticulatae Pericarpium.Conclusion:This work revealed that the intrinsic quality of Citri Reticulatae Pericarpium was affected by different growing regions,which provides a scientific basis for controlling the quality of Citri Reticulatae Pericarpium and rationally developing and utilizing Citri Reticulatae Pericarpium.
基金supported by the National Natural Science Foundation of China(No.82204276)the Guangxi Natural Science Foundation(No.2021GXNSFBA075036)+4 种基金the Specific Research Project of Guangxi for Research Bases and Talents(Nos.AD22035018,AD20297036)the 2021 University-Level Scientific Research Projects of Guangxi Minzu University(No.2021MDKJ003)the Talent Scientific Research Initiation Project of Guangxi Minzu University(No.2021KJQD09)the Xiangsi Lake Youth Innovation Team Project of Guangxi Minzu University(No.2021 RSCXSHQN01)the Guangxi Scholarship Fund of Guangxi Education Department.
文摘One new spirocyclic alkaloid,5-isopentenyl-cryptoechinuline D(1),along with 11 known compounds(2–12),were iso-lated from a marine fungus Aspergillus ruber TX-M4-1.The structures of compounds 1–12 were elucidated by spectroscopic evi-dences.Compound 1 was initially isolated as an enantiomer,and further separation of 1 by chiral HPLC afforded a pair of enantio-mers,including(-)-5-isopentenyl-cryptoechinuline D(1a)and(+)-5-isopentenyl-cryptoechinuline D(1b).Their absolute configura-tions were elucidated by ECD spectroscopic data.Compounds 1a,5 and 10 could inhibit thioredoxin reductase(TrxR)activity with IC50 values of 6.2,36.3 and 18.6μmol L^(-1),respectively.Surface plasmon resonance(SPR)study also demonsrated the interactions between compounds 6,8 and Niemann-Pick C1 Like 1(NPC1L1)respectively,which indicate that compounds 6 and 8 are potential NPC1L1 inhibitors.
基金supported by grants from the National Natural Science Foundation of China (No. 30600535 and No.30901288)
文摘Listeria monocytogenes(LM),a Gram-positive facultative intracellular bacterium,can be used as an effective exogenous antigen expression vector in tumor-target therapy.But for successful clinical application,it is necessary to construct attenuated LM stain that is safe yet retains the potency of LM based on the full virulent pathogen.In this study,attenuated LM and recombinants of LM expressing melanoma inhibitory activity(MIA) were constructed successfully.The median lethal dose(LD 50) and invasion efficiency of attenuated LM strains were detected.The recombinants were utilized for immunotherapy of animal model of B16F10 melanoma.The level of MIA mRNA expression in tumor tissue was detected by using real-time polymerase chain reaction(PCR) with specific sequence,meanwhile the anti-tumor immune response was assayed by flow cytometric analysis and enzyme-linked immunosorbent spot(ELISPOT) assay.The results showed the toxicity and invasiveness of attenuated LM were decreased as compared with LM,and attenuated LM expressing MIA,especially the double-genes attenuated LM recombinant,could significantly induce anti-tumor immune response and inhibit tumor growth.This study implicates attenuated LM may be a safer and more effective vector for immunotherapy of melanoma.
基金supported by the National Natural Science Foundation of China(No.81573550)。
文摘Steroid saponins are secondary metabolites with multiple medicinal values that are found in large quantities in natural medicines,especially Vernonia amygdalina,a famous nature medicine for the treatment of tonsillitis,diabetes,pneumonia.The current study was designed to combine molecular networking(MN)with diagnostic ions for rapid identification ofΔ^(7,9(11))stigmastane-type saponins which were theα-glucosidase inhibitory active substances in V.amygdalina.First,theα-glucosidase inhibitory activities of fiveΔ^(7,9(11))stigmastane-type steroid saponins that were previously isolated were screened,which indicated that theΔ^(7,9(11))stigmastane-type steroid saponin was one of the active constituents responsible for ameliorating diabetes.Furthermore,a strategy was proposed to identify stigmastane-type steroid saponins and verify the plausibility of derived fragmentation pathways by applying MN,MolNetEnhancer and unsupervised substructure annotation(MS2LDA).Based on this strategy,other sevenΔ^(7,9(11))stigmastane-type steroid saponins were identified from this plant.Our research provide scientific evidence for the antidiabetic potential of the steroid saponin-rich extract of V.amygdalina leaf.
基金supported by a program of the National Natural Science Foundation of China(Nos.31872675 and 81373288)the cooperation program between Chinese Academy of Sciences and Guangdong Province(2013B09110011).
文摘Ten cucurbitane-type triterpene glycosides,including five new compounds named charantosides H(1),J(2),K(3),momor-characoside A(4),goyaglycoside-l(5),and five known compounds(6-10),were isolated from the EtOAc extract of Momor-dica charantia fruits.The chemical structures of these compounds were identified by 1D and 2D NMR and HRESIMS spectroscopic analyses.Configurations of new compounds were determined by ROESY correlations and comparison of their 13C NMR data with literature reported values.All compounds were evaluated for their inhibition againstα-glucosidase,in which compounds 2,5,7,8,9 showed moderate inhibitory activities with IC50 values ranging from 28.40 to 63.26μM comparing with the positive control(acarbose,IC5087.65±6.51μM).
